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Compound Detail

CHEMBL480818

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CC[C@H](NC(=O)c1c(N)c(-c2ccccc2)nc2ccccc12)c1ccccc1

Basic Information

ChEMBL ID CHEMBL480818
Phase Preclinical
Structure Type MOL
InChI Key WHYVQTNGHLVEHF-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

381.5
MW (Da)
5.37
ALogP
3
HBA
2
HBD
68.0
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N3O
MW 381.48
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.82

Activity Summary

Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuromedin-K receptor
CHEMBL4429
Ki 8.7 8.7 2.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 577.0 ng.hr/g Rattus norvegicus
CL 27.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 80.0 ng/g Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuromedin-K receptor Ki = 1.995 nM 8.7 Binding affinity to NK3 receptor 19117759

Literature References

PubMed DOI Target Context # Activities
19117759 10.1016/j.bmcl.2008.12.005 Brain 2
19117759 10.1016/j.bmcl.2008.12.005 Rattus norvegicus 1
19117759 10.1016/j.bmcl.2008.12.005 Neuromedin-K receptor 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine